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Pharmacology How drugs affect the workings of the human body.

 
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  #1  
Old 23-11-2010, 16:11
Piglet Piglet is offline
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Ah-7921

Anti-nociceptive effects in N-substituted cyclohexylmethylbenzamides

This is a brief article on the totally synthetic, totally unrelated to any controlled compound, opioid analgesic AH-7921. Both the 3,4 dichloro & the N,N dimethyl are needed to produce a potent analgesic...


British journal of pharmacology 49 (1): 158P–159P

R. T. BRITrAIN, D. N. KELLETT, M. L. NEAT & R. STABLES

Department of Pharmacology, Allen & Hanburys Limited, Ware and Huntingdon Research Centre, Huntingdon.

In the mouse, certain N-substituted cyclohexylmethylbenzamides markedly inhibited writhing induced by phenylquinone and the nociceptive responses to being placed on a hot plate (Table 1). The results indicated that these compounds possessed analgesic activity and [3,4-dichloro-N-fl-(dimethylamino)cyclohexyl] methylbenzamide (AH 7921) was selected for detailed study in higher species.
In the conscious dog the minimal oral effective doses of AH 7921, morphine and codeine required to completely suppress the pain response to electrical stimulation of the dental pulp (Neat & Peacock, 1971) were 1.25±0.8, 1.25±0-3 and 3.5±0±6 mg/kg respectively. In a similar test using the conscious rhesus monkey the minimal antinociceptive doses of AH 7921, morphine and codeine were 13.8±1-2, <5.0 and 11.3±0.8 mg/kg espectively. Anti-nociceptive doses of AH 7921 caused no overt behavioural effects in the mouse, dog or monkey but higher doses (50 mg/kg orally) caused slight central nervous system depression. The addictive liability of AH 7921 was next investigated. AH 7921 was administered orally to rats, 5 mg/kg 3 times a day increasing to 20 mg/kg 3 times a day over 5 days. On the fifth day the animals were challenged with naloxone 0.25 mg/kg s.c., which caused an abstinence syndrome similar to that produced in animals that had received morphine on a similar dosage schedule. In the rhesus monkey single doses of AH 7921, 5-10 mg/kg s.c., completely alleviated the abstinence syndrome in morphine-dependent animals. In addition, AH 7921, 7-5 mg/kg s.c. twice daily, increasing to 30 mg/kg s.c. twice daily over 30 days, produced physical dependence in naive monkeys which was demonstrated in two ways. Nalorphine, 2 mg/kg s.c., induced an abstinence syndrome typical of that seen following morphine withdrawal in morphine-dependent monkeys. Secondly, on terminating AH 7921 treatment abstinence signs appeared over a period of 24-48 h. AH 7921 would be classed as a narcotic analgesic having high addictive liability. These findings are relevant to the relationship between structures of morphine-like compounds and addictive liability.

TABLE 1. Anti-nociceptive effects of some N-substituted cyclohexylmethylbenzamides in the mouse

R1-CONH.CH2 R2
Phenylquinone test Hot plate test
AH no. R, R2 ED50 mg/kg orally ED50 mg/kg s.c.
7563 -N(CH,)2 15-3 (7-6-31-0) 15-5 (5-4-42-0)
8533 2Cl -N(CH,)2 >100 60
8532 3Cl -N(CHS)2 16-0(8-4-34-0) 95 (4-3-24-5)

8529 4Cl -N(CH,)2 7-3(3-3-16-1) 50(1-7-15)
7921 3,4Cl -N(CHS)2 0-85 (0-4-1*7) 2-5 (1-2-6-4)

7959 3,4Cl piperidine >100 > 100
8507 3,4Cl N-methyl piperizine >100 >100

Morphine 11 (0-7-1-8) 2-8(1-1-48)
Codeine 5 8 (2-9-11-6) 17-0(9-1-32-0)

We would like to thank Dr. G. B. A. Veitch, University of Aston, Birmingham and the Research Chemists of the External Projects Unit, Allen & Hanburys Ltd., Ware for the synthesis of the compounds used in this work.

REFERENCE
NEAT, M. L. & PEACOCK, R. (1971). Implantation of electrodes in the dentine of an upper canine tooth in the dog. Br. J. Pharmac., 43, 476-477P.

Last edited by Piglet; 23-11-2010 at 16:14. Reason: Edit... I need to learn how to make tables!
  #2  
Old 24-11-2010, 17:48
Piglet Piglet is offline
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Re: Ah-7921

SWIM should point out that this stuff can be synthesised in a single step from commercially available & non-suspicious chemicals... and it's equipotent with morphine.
  #3  
Old 24-11-2010, 20:50
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Re: Ah-7921

How does its lipid solubility compare?
  #4  
Old 24-11-2010, 21:08
Valseedian Valseedian is offline
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Re: Ah-7921

Quote:
Originally Posted by Piglet View Post
SWIM should point out that this stuff can be synthesised in a single step from commercially available & non-suspicious chemicals... and it's equipotent with morphine.
care to share the tek? Ive UTFSE with no luck...
swim is very interested.
  #5  
Old 24-11-2010, 23:20
sam o sam o is offline
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Re: Ah-7921

Very interesting chemical, I'v done research with analgesic peptides mainly ones that pass the BBB , in hope to find a stable one with a long duration.
Dermorphin seems to fit the bill

If AH-7921 is on parr with morphine would the starting dosage and duration be basically the same?

Anyone want to take a guess with AH-7921 , passing all drug screenings(GS/MS) ?

Thanks.
  #6  
Old 25-11-2010, 11:28
Piglet Piglet is offline
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Re: Ah-7921

Will it pass blood-screenings? - YES!

Lipid solubility? - partition coefficient unreported but onset/duration similar to morphine & very active orally. The Ki isn't actually that great but the compound is 'highly lipophilic' so the concentration in the brain will be high compared with M.

Addictive Liability? - Low (Straub Index)

Synthesis? - It's an amide: Find the appropriate acid chloride & (di)amine: they ARE out there & easy to find (SWIM took 60 seconds). Schotten–Baumann type synthesis was used by Dr. G. B. A. Veitch. Sadly the good doctor is no longer with us so SWIM cannot ask for details!

Last edited by Piglet; 25-11-2010 at 11:56.
  #7  
Old 25-11-2010, 13:16
sam o sam o is offline
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Re: Ah-7921

What would be a good starting dosage based on the abstract listed above(orally and i.v.)
Do you think most of the studies were done using AH-7921 in it's hydrochloride form? (I see that wikipedia also has info. on it's hcl form)

Thanks
  #8  
Old 25-11-2010, 15:59
Jasim Gold member Jasim is offline
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Re: Ah-7921

Quote:
Originally Posted by sam o View Post
If AH-7921 is on parr with morphine would the starting dosage and duration be basically the same?
I just want to point out that the comment regarding dosage is NOT a valid assertion with any substance. Dosage and efficacy are two completely different concepts in pharmacology. A drug can have an identical efficacy, but vary dramatically in the dosage require to meet that effect. This would be a variance in potency.

Regardless, with any research chemical without good documentation on human dosages one should take extreme caution and increase dose slowly with a starting dose well below the expected threshold for any noticeable effect.
  #9  
Old 25-11-2010, 21:14
sam o sam o is offline
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Re: Ah-7921

Quote:
Originally Posted by Jasim View Post
I just want to point out that the comment regarding dosage is NOT a valid assertion with any substance. Dosage and efficacy are two completely different concepts in pharmacology. A drug can have an identical efficacy, but vary dramatically in the dosage require to meet that effect. This would be a variance in potency.

Regardless, with any research chemical without good documentation on human dosages one should take extreme caution and increase dose slowly with a starting dose well below the expected threshold for any noticeable effect.

I understand your concerns ,but I have NO intention on trying this chemical, just a hypothetical thats all.

I appreciate your post thou.
  #10  
Old 13-11-2011, 09:14
DynoMiTe DynoMiTe is offline
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Re: Ah-7921

Any more info on this? My Buddha statue has been looking into a custom synthesis of this but I do not want to jump in with out knowing more about it.
  #11  
Old 10-03-2012, 01:55
DynoMiTe DynoMiTe is offline
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Re: Ah-7921

I know SWIM was the last one to post. SWIM will have this tomorrow. It is getting sent straight away to a lab to get testing with GC/MS and HPLC. SWIM will post the results ASAP.
  #12  
Old 13-03-2012, 03:45
xJSL xJSL is offline
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Re: Ah-7921

Quote:
Originally Posted by Piglet View Post
Addictive Liability? - Low (Straub Index)
Just wondering, why would the addiction liability of a drug like this be low? I mean, any drug that can bind to the mu opioid receptor with a similar potency as morphine is bound to be pretty addictive.
  #13  
Old 11-07-2012, 22:30
Alfa Alfa is offline
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Re: Ah-7921

AH-7921 seems to be going around now. More information would be welcome.
  #14  
Old 21-07-2012, 09:28
Lady Codone Lady Codone is offline
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Re: Ah-7921

SWIM will likely be trying some of this soon and would appreciate any/all advice she can get. Is the high more similar to opium/hydrocodone (heavy, sedating) or oxycodone (stimulating/energetic)? How is it on side effects like nausea and dizziness? What's a relatively safe starting dose for an opiate-naive researcher?

From reading, it appears that sublingual is the best ROA...right?

So much to learn!
  #15  
Old 26-08-2012, 12:51
Baba Blacksheep Baba Blacksheep is offline
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Re: Ah-7921

Moved to Experiences.

Last edited by Baba Blacksheep; 26-08-2012 at 20:24.
  #16  
Old 28-11-2012, 10:19
Rob Cypher Rob Cypher is offline
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Re: Ah-7921

None of the reports I've read on DF or other forums have been very positive about this substance - it appears less effective than tramadol unless you go into the 200-500 mg range, and then there's a chance of sudden OD around that range (especially when mixed with other things, as some are want to do). I'd avoid just based on word of mouth alone.

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ah-7921, opiate analogues, opioid analogues, opioid chemistry, opioid research chemicals, opioids

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